EP 2262771 A1 20101222 - A METHOD FOR THE PREPARATION OF DABIGATRAN
Title (en)
A METHOD FOR THE PREPARATION OF DABIGATRAN
Title (de)
VERFAHREN ZUR HERSTELLUNG VON DABIGATRAN
Title (fr)
PROCÉDÉ DE PRÉPARATION DE DABIGATRAN
Publication
Application
Priority
- CZ 2009000037 W 20090310
- CZ 2008165 A 20080314
Abstract (en)
[origin: WO2009111997A1] A method for the manufacture of dabigatran of formula VIII, in which the product of a reaction of 4-ethylamino-3-nitrobenzoic acid chloride with ethyl-3-(pyridin-2- ylamino)propanoate, is converted to the hydrochloride using a hydrogen chloride solution producing the compound of formula III-HC1, in which the nitro group is reduced by means of a reaction with sodium dithionite, and the resulting compound of formula IV is subjected to a reaction with [(4-cyanophenyl)amino] acetic acid and oxalic acid, the product of this reaction Vl-oxal is then subjected to hydrolysis and a reaction with ammonium carbonate to produce the intermediate of formula VII-HCl, which is then converted to dabigatran by means of a reaction with hexyl chloroformate.
IPC 8 full level
C07D 213/74 (2006.01); C07D 401/12 (2006.01)
CPC (source: EP US)
C07D 213/74 (2013.01 - EP US); C07D 401/12 (2013.01 - EP US)
Citation (search report)
See references of WO 2009111997A1
Designated contracting state (EPC)
AT BE BG CH CY CZ DE DK EE ES FI FR GB GR HR HU IE IS IT LI LT LU LV MC MK MT NL NO PL PT RO SE SI SK TR
Designated extension state (EPC)
AL BA RS
DOCDB simple family (publication)
WO 2009111997 A1 20090917; CZ 2008165 A3 20090923; CZ 305085 B6 20150429; EA 018053 B1 20130530; EA 201001394 A1 20110228; EP 2262771 A1 20101222; UA 102248 C2 20130625; US 2011082299 A1 20110407; US 8394961 B2 20130312
DOCDB simple family (application)
CZ 2009000037 W 20090310; CZ 2008165 A 20080314; EA 201001394 A 20090310; EP 09719117 A 20090310; UA A201012170 A 20090310; US 92221409 A 20090310